N-to-C solid-phase peptide and peptide trifluoromethylketone synthesis using amino acid tert-butyl esters |
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Authors: | Gutheil William G Xu Qingchai |
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Affiliation: | Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City, 64110, USA. gutheilw@umkc.edu |
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Abstract: | Solid-phase peptide synthesis in the N-to-C direction, opposite to the classical C-to-N direction of peptide synthesis, provides the synthetically versatile C-terminal carboxyl group for further modification into C-terminally modified peptide mimetics. These are of general interest as potential bioactive agents, particularly as protease inhibitors. Elaboration of peptide mimetics on the solid-phase would facilitate synthesis of peptide mimetic combinatorial libraries. This report describes an effective strategy for solid-phase inverse peptide synthesis based on readily available amino acid tert-butyl esters. The potential of this approach for peptide mimetic synthesis is demonstrated by the solid-phase synthesis of two peptide trifluoromethylketones. |
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